ArticleBioorganic & medicinal chemistry2012
Design, synthesis, biochemical studies, cellular characterization, and structure-based computational studies of small molecules targeting the urokinase receptor.
Article in Bioorganic & medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed, 42 citations in OpenAlex.
- Review
- Review
- Design and Synthesis of Fragment Derivatives with a Unique Inhibition Mechanism of the uPAR·uPA Interaction.ACS medicinal chemistry letters · 2021Article
- Unconventional Secondary Structure Mimics: Ladder-Rungs.Angewandte Chemie (International ed. in English) · 2020Article
- Structures, functions, and mechanisms of filament forming enzymes: a renaissance of enzyme filamentation.Biophysical reviews · 2019Review
- Proteolysis is the most fundamental property of malignancy and its inhibition may be used therapeutically (Review).International journal of molecular medicine · 2019Review
- Can components of the plasminogen activation system predict the outcome of kidney transplants?Central-European journal of immunology · 2018Review
- Article
- Small Molecules Engage Hot Spots through Cooperative Binding To Inhibit a Tight Protein-Protein Interaction.Biochemistry · 2017Article
- Urokinase type plasminogen activator receptor (uPAR) as a new therapeutic target in cancer.Translational medicine @ UniSa · 2016Article
- Re-engineering the Immune Response to Metastatic Cancer: Antibody-Recruiting Small Molecules Targeting the Urokinase Receptor.Angewandte Chemie (International ed. in English) · 2016Article
- A new class of orthosteric uPAR·uPA small-molecule antagonists are allosteric inhibitors of the uPAR·vitronectin interaction.ACS chemical biology · 2015Article
- Preparation and antitumor effect of a toxin-linked conjugate targeting vascular endothelial growth factor receptor and urokinase plasminogen activator.Experimental biology and medicine (Maywood, N.J.) · 2015Article
- Preclinical evaluation of a urokinase plasminogen activator receptor-targeted nanoprobe in rhesus monkeys.International journal of nanomedicine · 2015Article
- Nonanebis(peroxoic acid): a stable peracid for oxidative bromination of aminoanthracene-9,10-dione.Beilstein journal of organic chemistry · 2014Article
- Probing binding and cellular activity of pyrrolidinone and piperidinone small molecules targeting the urokinase receptor.ChemMedChem · 2013Article
- Small-molecule inhibition of the uPAR·uPA interaction: synthesis, biochemical, cellular, in vivo pharmacokinetics and efficacy studies in breast cancer metastasis.Bioorganic & medicinal chemistry · 2013Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
The urokinase receptor (uPAR) serves as a docking site to the serine protease urokinase-type plasminogen activator (uPA) to promote extracellular matrix (ECM) degradation and tumor invasion and metastasis. Previously, we had reported a small molecule inhibitor of the uPAR·uPA interaction that emerged from structure-based virtual screening. Here, we measure the affinity of a large number of derivatives from commercial sources. Synthesis of additional compounds was carried out to probe the role of various groups on the parent compound. Extensive structure-based computational studies suggested a binding mode for these compounds that led to a structure-activity relationship study. Cellular studies in non-small cell lung cancer (NSCLC) cell lines that include A549, H460 and H1299 showed that compounds blocked invasion, migration and adhesion. The effects on invasion of active compounds were consistent with their inhibition of uPA and MMP proteolytic activity. These compounds showed weak cytotoxicity consistent with the confined role of uPAR to metastasis.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.